Synthesis and functional screening of novel inhibitors targeting the HDAC6 zinc finger ubiquitin-binding domain

Authors: Geurs, Silke ^{a, b}, Staessens, Eleni ^{b, c, d}, Bredael, Kato ^a, Borghgraef, Stefaan ^a, De Ridder, Jordy ^a, Persoons, Leentje ^e, De Jonghe, Steven ^f, Schols, Dominique ^f, Mann, Mandeep K. ^g, Harding, Rachel J. ^{g, h, i}, Franceus, Jorick ^j, Desmet, Tom ^j, Van Hecke, Kristof ^k, Clarisse, Dorien ^{b, c, d, ⁎⁎}, De Bosscher, Karolien ^{b, c, d, ⁎⁎⁎}, D'hooghe, Matthias ^{a, d, ⁎}

Source: In European Journal of Medicinal Chemistry 5 March 2025 285

Synthesis of 3-heteroaryl-pyrrolo[2,3-b]pyridines as potent inhibitors of AP-2-associated protein kinase 1 (AAK1) with antiviral activity

Authors: Ravi, Nitha Panikkassery, Van Eynde, Wout, Karim, Marwah, Nhu Tran, Do Hoang, Agrawal, Aditi, Schols, Dominique, Voet, Arnout, Einav, Shirit, Dehaen, Wim, De Jonghe, Steven

Source: In European Journal of Medicinal Chemistry 15 December 2024 280

Steroidal 21-imidazolium salt derivatives: Synthesis and anticancer activity

Authors: Sucman, Natalia S., Ya. Bilan, Dmitri, Cojocari, Sergiu V., Pogrebnoi, Vsevolod S., Stîngaci, Eugenia P., Khripach, Vladimir A., Zhabinskii, Vladimir N., Tsybruk, Tatsiana V., Grabovec, Irina P., Panibrat, Olesya V., Persoons, Leentje, Schols, Dominique, Froeyen, Mathy, Shova, Sergiu, De Jonghe, Steven, Macaev, Fliur Z.

Source: In Steroids October 2024 210

Identification of novel human CC chemokine receptor 8 (CCR8) antagonists via the synthesis of naphthalene amide and sulfonamide isosteres

Authors: Verhaegen, Yenthel, Liu, Libao, Nguyen, Tien T., Loy, Tom Van, Schols, Dominique, Voet, Arnout R.D., Dehaen, Wim, De Jonghe, Steven

Source: In Bioorganic Chemistry April 2024 145

Synthesis and cancer cell cytotoxicity of 2-heteroaryl-4-(4-heteroaryl-2-oxobut-3-en-1-ylidene)-substituted benzothiazepanes

Authors: Magdalenić, Katarina, Morlion, Felien, De Jonghe, Steven, Persoons, Leentje, Schols, Dominique, Grootaert, Charlotte, Van Camp, John, D'hooghe, Matthias

Source: In Tetrahedron 25 March 2024 154

Design, synthesis, and molecular modeling studies of novel 2-quinolone-1,2,3-triazole-α-aminophosphonates hybrids as dual antiviral and antibacterial agents

Authors: Gadali, Khadija El, Rafya, Meriem, El Mansouri, Az-eddine, Maatallah, Mohamed, Vanderlee, Arie, Mehdi, Ahmad, Neyts, Johan, Jochmans, Dirk, De Jonghe, Steven, Benkhalti, Fatiha, Sanghvi, Yogesh S., Taourirte, Moha, Lazrek, Hassan B.

Source: In European Journal of Medicinal Chemistry 15 March 2024 268

Photo-induced scandium-catalyzed biomimetic skeleton conversion of lathyrane to naturally rare eupholathone Euphorbia diterpenesElectronic supplementary information (ESI) available. CCDC 2254435 and 2254434. For ESI and crystallographic data in CIF or other electronic format see DOI: https://doi.org/10.1039/d3cc03541g

Authors: Xu, Jin-Bu, Wen, Peng, Wang, Neng, Li, Xiaohuan, Li, Jia-Hong, De Jonghe, Steven, Schols, Dominique, Chen, Feng-Zheng, Gao, Feng

Source: Chemical communications. 59(82):12290-12293

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100195578153.0x000001&indx=1&recIds=ETOCvdc_100195578153.0x000001

Synthesis and cancer cell cytotoxicity of 2-aryl-4-(4-aryl-2-oxobut-3-en-1-ylidene)-substituted benzothiazepanes

Authors: Magdalenić, Katarina, Ronse, Ulrike, De Jonghe, Steven, Persoons, Leentje, Schols, Dominique, De Munck, Julie, Grootaert, Charlotte, Van Camp, John, D'hooghe, Matthias

Source: Phytochemistry letters. 55:117-123

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100191928801.0x000001&indx=1&recIds=ETOCvdc_100191928801.0x000001

Visible-Light-Promoted Tandem Thiol—Ene Click Reaction/Transannular Cyclization and Regioselective Cyclopropane Ring-Opening to Construct Sulfur-Containing Euphorbia Diterpenes

Authors: Wang, Neng, Wang, Hang, Wan, Lin-Xi, Li, Xiao-Huan, Zhou, Xian-Li, Li, Jia-Hong, De Jonghe, Steven, Schols, Dominique, Xu, Jin-Bu, Gao, Feng

Source: Organic letters. 25(4):597-602

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCRN631757709&indx=1&recIds=ETOCRN631757709

Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cellsElectronic supplementary information (ESI) available. See DOI: https://doi.org/10.1039/d2sc04147b

Authors: Vanhoutte, Roeland, Barniol-Xicota, Marta, Chiu, Winston, Vangeel, Laura, Jochmans, Dirk, De Jonghe, Steven, Zidane, Hadeer, Barr, Haim M., London, Nir, Neyts, Johan, Verhelst, Steven H. L.

Source: Chemical science. 14(7):1666-1672

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100173876909.0x000001&indx=1&recIds=ETOCvdc_100173876909.0x000001

Synthesis and structure–activity relationship study of phenoxybenzylpiperazine analogues as CCR8 agonists

Authors: Li, Qifei, Claes, Sandra, Verhaegen, Yenthel, Anthonissen, Stijn, Van Loy, Tom, Schols, Dominique, Dehaen, Wim, De Jonghe, Steven

Source: In Bioorganic Chemistry October 2023 139

Development of a robust and convenient dual-reporter high-throughput screening assay for SARS-CoV-2 antiviral drug discovery

Authors: Chiu, Winston, Schepers, Joost, Francken, Thibault, Vangeel, Laura, Abbasi, Kayvan, Jochmans, Dirk, De Jonghe, Steven, Thibaut, Hendrik Jan, Thiel, Volker, Neyts, Johan, Laporte, Manon, Leyssen, Pieter

Source: In Antiviral Research February 2023 210

Synthesis, characterization, molecular docking, and anticancer activities of new 1,3,4-oxadiazole-5-fluorocytosine hybrid derivatives

Authors: El Mansouri, Az-eddine, Lachhab, Saida, Oubella, Ali, Mehdi, Ahmad, Neyts, Johan, Jochmans, Dirk, Chiu, Winston, Vangeel, Laura, De Jonghe, Steven, Morjani, Hamid, Ali, Mustapha Ait, Zahouily, Mohamed, Sanghvi, Yogesh S., Lazrek, Hassan B.

Source: In Journal of Molecular Structure 15 January 2023 1272

Development and optimization of a high‐throughput screening assay for in vitro anti‐SARS‐CoV‐2 activity: Evaluation of 5676 Phase 1 Passed Structures

Authors: Chiu, Winston, Verschueren, Lore, Van den Eynde, Christel, Buyck, Christophe, De Meyer, Sandra, Jochmans, Dirk, Bojkova, Denisa, Ciesek, Sandra, Cinatl, Jindrich, De Jonghe, Steven, Leyssen, Pieter, Neyts, Johan, Van Loock, Marnix, Van Damme, Ellen

Source: Journal of medical virology. 94(7):3101-3111

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100191768953.0x000001&indx=1&recIds=ETOCvdc_100191768953.0x000001

Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses

Authors: Luttens, Andreas, Gullberg, Hjalmar, Abdurakhmanov, Eldar, Vo, Duy Duc, Akaberi, Dario, Talibov, Vladimir O., Nekhotiaeva, Natalia, Vangeel, Laura, De Jonghe, Steven, Jochmans, Dirk

Source: Journal of the American Chemical Society. 144(7):2905-2920

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCRN628718397&indx=1&recIds=ETOCRN628718397

The discovery of Zika virus NS2B-NS3 inhibitors with antiviral activity via an integrated virtual screening approach

Authors: Mirza, Muhammad Usman, Alanko, Ida, Vanmeert, Michiel, Muzzarelli, Kendall M., Salo-Ahen, Outi M.H., Abdullah, Iskandar, Kovari, Iulia A., Claes, Sandra, De Jonghe, Steven, Schols, Dominique, Schinazi, Raymond F., Kovari, Ladislau C., Trant, John F., Ahmad, Sarfraz, Froeyen, Matheus

Source: In European Journal of Pharmaceutical Sciences 1 August 2022 175

Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies

Authors: Karim, Marwah, Saul, Sirle, Ghita, Luca, Sahoo, Malaya Kumar, Ye, Chengjin, Bhalla, Nishank, Lo, Chieh-Wen, Jin, Jing, Park, Jun-Gyu, Martinez-Gualda, Belén, East, Michael Patrick, Johnson, Gary L., Pinsky, Benjamin A., Martinez-Sobrido, Luis, Asquith, Christopher R.M., Narayanan, Aarthi, De Jonghe, Steven, Einav, Shirit

Source: In Antiviral Research August 2022 204

Discovery of (3-Phenylcarbamoyl-3,4-dihydro‑2H‑pyrrol-2-yl)phosphonates as Imidazoline I2 Receptor Ligands with Anti-Alzheimer and Analgesic Properties.

Authors: Bagán, Andrea, López-Ruiz, Alba, Abás, Sònia, Ruiz-Cantero, M. Carmen, Vasilopoulou, Foteini, Taboada-Jara, Teresa, Griñán-Ferré, Christian, Pallàs, Mercè, Muguruza, Carolina, Diez-Alarcia, Rebeca, Callado, Luis F., Entrena, José M., Cobos, Enrique J., Pérez, Belén, Morales-García, José A., Molins, Elies, De Jonghe, Steven, Daelemans, Dirk, Brea, José, Val, Cristina

Source: Journal of Medicinal Chemistry; 2/13/2025, Vol. 68 Issue 3, p2551-2573, 23p

Optimization of SARS-CoV-2 M pro Inhibitors by a Structure-Based Multilevel Virtual Screening Method.

Authors: Jing, Lanlan, Zhao, Fabao, Zheng, Lin, Meng, Bairu, Gao, Shenghua, Laporte, Manon, Jochmans, Dirk, De Jonghe, Steven, Neyts, Johan, Zhan, Peng, Kang, Dongwei, Liu, Xinyong

Source: International Journal of Molecular Sciences; Jan2025, Vol. 26 Issue 2, p670, 19p

Subject Terms: VIRTUAL high-throughput screening (Drug development), MOLECULAR dynamics, DRUG development, SARS-CoV-2, COVID-19

HIV protease inhibitors Nelfinavir and Lopinavir/Ritonavir markedly improve lung pathology in SARS-CoV-2-infected Syrian hamsters despite lack of an antiviral effect

Authors: Foo, Caroline S., Abdelnabi, Rana, Kaptein, Suzanne J.F., Zhang, Xin, ter Horst, Sebastiaan, Mols, Raf, Delang, Leen, Rocha-Pereira, Joana, Coelmont, Lotte, Leyssen, Pieter, Dallmeier, Kai, Vergote, Valentijn, Heylen, Elisabeth, Vangeel, Laura, Chatterjee, Arnab K., Annaert, Pieter P., Augustijns, Patrick F., De Jonghe, Steven, Jochmans, Dirk, Gouwy, Mieke, Cambier, Seppe, Vandooren, Jennifer, Proost, Paul, van Laer, Christine, Weynand, Birgit, Neyts, Johan

Source: In Antiviral Research June 2022 202